JP2014516070A5 - - Google Patents
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- Publication number
- JP2014516070A5 JP2014516070A5 JP2014514056A JP2014514056A JP2014516070A5 JP 2014516070 A5 JP2014516070 A5 JP 2014516070A5 JP 2014514056 A JP2014514056 A JP 2014514056A JP 2014514056 A JP2014514056 A JP 2014514056A JP 2014516070 A5 JP2014516070 A5 JP 2014516070A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- cycloalkyl
- heterocyclyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000001424 substituent group Chemical group 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 32
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 229910052799 carbon Inorganic materials 0.000 claims description 28
- 150000001875 compounds Chemical class 0.000 claims description 27
- 229910052717 sulfur Inorganic materials 0.000 claims description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 229910052760 oxygen Inorganic materials 0.000 claims description 20
- 125000005842 heteroatom Chemical group 0.000 claims description 16
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 12
- -1 heterocyclyl-O— Chemical group 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 125000002837 carbocyclic group Chemical group 0.000 claims description 10
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 8
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 8
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims description 6
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims description 6
- 230000004913 activation Effects 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000001624 naphthyl group Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 239000000969 carrier Substances 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 0 CC(C)(C1)CN(*)CCC1N(C1CC1)C(*[Al]=C)=O Chemical compound CC(C)(C1)CN(*)CCC1N(C1CC1)C(*[Al]=C)=O 0.000 description 9
- 238000000034 method Methods 0.000 description 2
- GGTZFVAIGQEKIK-UHFFFAOYSA-O CC([NH2+]C)=NC=N Chemical compound CC([NH2+]C)=NC=N GGTZFVAIGQEKIK-UHFFFAOYSA-O 0.000 description 1
- WCGNLBCJPBKXCN-UHFFFAOYSA-N Cc(cc1)cc(F)c1C#N Chemical compound Cc(cc1)cc(F)c1C#N WCGNLBCJPBKXCN-UHFFFAOYSA-N 0.000 description 1
- KUQQONVKIURIQU-UHFFFAOYSA-N Cc(ccc(C#N)c1)c1F Chemical compound Cc(ccc(C#N)c1)c1F KUQQONVKIURIQU-UHFFFAOYSA-N 0.000 description 1
- RNHKXHKUKJXLAU-UHFFFAOYSA-N Cc1ccc(CC#N)cc1 Chemical compound Cc1ccc(CC#N)cc1 RNHKXHKUKJXLAU-UHFFFAOYSA-N 0.000 description 1
- GIWQSPITLQVMSG-UHFFFAOYSA-N Cc1ncc[n]1C Chemical compound Cc1ncc[n]1C GIWQSPITLQVMSG-UHFFFAOYSA-N 0.000 description 1
- 238000007792 addition Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11169297 | 2011-06-09 | ||
| EP11169297.6 | 2011-06-09 | ||
| PCT/EP2012/060729 WO2012168315A1 (en) | 2011-06-09 | 2012-06-06 | Substituted piperidines as gpr119 modulators for the treatment of metabolic disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014516070A JP2014516070A (ja) | 2014-07-07 |
| JP2014516070A5 true JP2014516070A5 (enExample) | 2015-07-23 |
| JP6094578B2 JP6094578B2 (ja) | 2017-03-15 |
Family
ID=46245574
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014514056A Active JP6094578B2 (ja) | 2011-06-09 | 2012-06-06 | 代謝性障害の治療のためのｇｐｒ１１９モジュレーターとしての置換ピペリジン |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8921398B2 (enExample) |
| EP (1) | EP2718288B1 (enExample) |
| JP (1) | JP6094578B2 (enExample) |
| AR (1) | AR086895A1 (enExample) |
| WO (1) | WO2012168315A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012123449A1 (en) | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
| US8921398B2 (en) | 2011-06-09 | 2014-12-30 | Boehringer Ingelheim International Gmbh | N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof |
| AU2013290100A1 (en) | 2012-07-11 | 2015-01-29 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| JP2015523404A (ja) | 2012-08-02 | 2015-08-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｎ−シクロプロピル−ｎ−ピペリジニル−アミド、これらを含有する医薬組成物およびその使用 |
| BR112015006696A2 (pt) * | 2012-09-25 | 2017-07-04 | Bayer Cropscience Ag | 3-fenilisoxazolina-5-carboxamidas 5-oxi-substituídas e 3-fenilisoxazolina-5-tioamidas 5-oxi-substituídas herbicidas e fungicidas |
| EP3490986B1 (en) | 2016-07-28 | 2021-11-24 | Idorsia Pharmaceuticals Ltd | Piperidine cxcr7 receptor modulators |
| KR102502046B1 (ko) | 2018-01-26 | 2023-02-20 | 이도르시아 파마슈티컬스 리미티드 | Cxcr7 수용체 작동제 (3s,4s)-1-시클로프로필메틸-4-｛[5-(2,4-디플루오로-페닐)-이속사졸-3-카르보닐]-아미노｝-피페리딘-3-카르복실산 (1-피리미딘-2-일-시클로프로필)-아미드의 결정질 형태 |
| EP3919489A4 (en) * | 2019-01-31 | 2022-10-12 | The National Institutes of Pharmaceutical R&D Co., Ltd | AROMATIC RING OR HETEROAROMATIC RING COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND MEDICAL USE |
| WO2025128834A1 (en) * | 2023-12-15 | 2025-06-19 | Alterome Therapeutics, Inc. | Akt1 modulators |
| TW202602878A (zh) * | 2024-03-27 | 2026-01-16 | 美商亞特羅姆醫療公司 | Ａｋｔ１調節劑 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI326214B (en) | 2002-07-17 | 2010-06-21 | Avanir Pharmaceuticals Inc | Pharmaceutical compositions comprising dextromethorphan and quinidine for the treatment of neurological disorders |
| US20060252797A1 (en) | 2002-11-06 | 2006-11-09 | Masahiro Kajino | Receptor regulator |
| US20070032475A1 (en) | 2005-04-15 | 2007-02-08 | Ye Xiaocong M | Novel compounds useful for bradykinin B1 receptor antagonism |
| BRPI0616575A2 (pt) * | 2005-09-27 | 2011-06-21 | Irm Llc | compostos e composições contendo diarilamina, seu uso como moduladores de receptores de c-kit bem como método para sua produção |
| US8039458B2 (en) | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| ATE476418T1 (de) * | 2006-06-08 | 2010-08-15 | Amgen Inc | Benzamidderivate und assoziierte verwendungen |
| EP2059517A1 (en) | 2006-08-30 | 2009-05-20 | Biovitrum AB (publ) | Pyrimidine compounds for treating gpr119 related disorders |
| DE602008002733D1 (de) | 2007-03-08 | 2010-11-04 | Irm Llc | Verbindungen und zusammensetzungen als modulatoren der gpr119-aktivität |
| GB0812648D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812649D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| AU2009330821B2 (en) * | 2008-12-24 | 2015-06-11 | Bial - Portela & Ca, S.A. | Pharmaceutical compounds |
| US8293729B2 (en) | 2009-06-24 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| JP5794297B2 (ja) | 2010-05-07 | 2015-10-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｇｐｒ１１９アゴニストとしてのピリダジノン |
| UY33805A (es) | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| UY33871A (es) | 2011-01-21 | 2012-07-31 | Boehringer Ingelheim Int | Compuestos y formulaciones farmacéuticas basadas en derivados de benzo y heteroarilos condensados 2,3-dihidrofurán-2-il-piperidina y sus usos |
| WO2012123449A1 (en) | 2011-03-14 | 2012-09-20 | Boehringer Ingelheim International Gmbh | N- cyclopropyl - n- piperidinylbenzamides as gpr119 modulators |
| US8921398B2 (en) | 2011-06-09 | 2014-12-30 | Boehringer Ingelheim International Gmbh | N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof |
-
2012
- 2012-06-06 US US13/489,557 patent/US8921398B2/en active Active
- 2012-06-06 JP JP2014514056A patent/JP6094578B2/ja active Active
- 2012-06-06 EP EP12726611.2A patent/EP2718288B1/en active Active
- 2012-06-06 WO PCT/EP2012/060729 patent/WO2012168315A1/en not_active Ceased
- 2012-06-08 AR ARP120102062A patent/AR086895A1/es unknown
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